Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor
PC Wong, DJP Pinto, D Zhang - Journal of thrombosis and thrombolysis, 2011 - Springer
Abstract Apixaban (BMS-562247; 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)
phenyl)-4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4-c] pyridine-3-carboxamide), a direct inhibitor …
phenyl)-4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4-c] pyridine-3-carboxamide), a direct inhibitor …
Catalytic Asymmetric Synthesis of Enantioenriched Heterocycles Bearing a CCF3 Stereogenic Center
YY Huang, X Yang, Z Chen, F Verpoort… - … –A European Journal, 2015 - Wiley Online Library
Given the important agricultural and medicinal application of optically pure heterocycles
bearing a trifluoromethyl group at the stereogenic carbon center in the heterocyclic …
bearing a trifluoromethyl group at the stereogenic carbon center in the heterocyclic …
Discovery of 1-[3-(Aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)- [1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a Highly …
DJP Pinto, MJ Orwat, S Wang, JM Fevig… - Journal of medicinal …, 2001 - ACS Publications
Factor Xa (fXa) plays a critical role in the coagulation cascade, serving as the point of
convergence of the intrinsic and extrinsic pathways. Together with nonenzymatic cofactor Va …
convergence of the intrinsic and extrinsic pathways. Together with nonenzymatic cofactor Va …
Discovery of 1-(3'-Aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide …
ML Quan, PYS Lam, Q Han, DJP Pinto… - Journal of medicinal …, 2005 - ACS Publications
Modification of a series of pyrazole factor Xa inhibitors to incorporate an
aminobenzisoxazole as the P1 ligand resulted in compounds with improved selectivity for …
aminobenzisoxazole as the P1 ligand resulted in compounds with improved selectivity for …
Enantioselective synthesis of trifluoromethyl‐substituted 2‐isoxazolines: asymmetric hydroxylamine/enone cascade reaction
K Matoba, H Kawai, T Furukawa, A Kusuda… - Angewandte Chemie …, 2010 - infona.pl
Cuts both ways: The title reaction consists of an addition/cyclization/dehydration sequence
and affords the biologically important chiral 3, 5‐diaryl‐5‐(trifluoromethyl)‐2‐isoxazolines 1 …
and affords the biologically important chiral 3, 5‐diaryl‐5‐(trifluoromethyl)‐2‐isoxazolines 1 …
Discovery, development, chemical diversity and design of isoxazoline-based insecticides
IL Gonçalves, GM das Neves, LP Kagami… - Bioorganic & Medicinal …, 2021 - Elsevier
Isoxazoline is a 5-membered heterocycle present in the active compounds of many
commercial veterinary anti-ectoparasitic products. The molecular target of isoxazolines is the …
commercial veterinary anti-ectoparasitic products. The molecular target of isoxazolines is the …
New anticoagulant drugs
JI Weitz - Journal of thrombosis and thrombolysis, 2001 - Springer
Arterial and venous thrombosis are major causes of morbidity and mortality. Arterial
thrombosis is the most common cause of myocardial infarction, stroke, and limb gangrene …
thrombosis is the most common cause of myocardial infarction, stroke, and limb gangrene …
Berotralstat (BCX7353): structure-guided design of a potent, selective, and oral plasma kallikrein inhibitor to prevent attacks of hereditary angioedema (HAE)
PL Kotian, M Wu, S Vadlakonda… - Journal of Medicinal …, 2021 - ACS Publications
Hereditary angioedema (HAE) is a rare and potentially life-threatening disease that affects
an estimated 1 in 50 000 individuals worldwide. Until recently, prophylactic HAE treatment …
an estimated 1 in 50 000 individuals worldwide. Until recently, prophylactic HAE treatment …
Contribution of in vivo models of thrombosis to the discovery and development of novel antithrombotic agents
RJ Leadley Jr, L Chi, SS Rebello, A Gagnon - Journal of pharmacological …, 2000 - Elsevier
Cardiovascular and cerebrovascular diseases continue to be the leading cause of death
throughout the world. Over the past two decades, great advances have been made in the …
throughout the world. Over the past two decades, great advances have been made in the …
Design and Quantitative Structure−Activity Relationship of 3-Amidinobenzyl-1H-indole-2-carboxamides as Potent, Nonchiral, and Selective Inhibitors of Blood …
H Matter, E Defossa, U Heinelt, PM Blohm… - Journal of Medicinal …, 2002 - ACS Publications
A series of 138 nonchiral 3-amidinobenzyl-1 H-indole-2-carboxamides and analogues as
inhibitors of the blood coagulation enzyme factor Xa (fXa) were designed, synthesized, and …
inhibitors of the blood coagulation enzyme factor Xa (fXa) were designed, synthesized, and …